128102-16-9

Usage

Uses

Used in Pharmaceutical Research:
(R)-2-METHYL-PIPERAZINE-1,4-DICARBOXYLIC ACID 4-BENZYL ESTER 1-TERT-BUTYL ESTER is used as a research compound for the development of new drugs, leveraging its unique chemical properties to explore its potential therapeutic effects and mechanisms of action.
Used in Organic Synthesis:
In the field of organic synthesis, (R)-2-METHYL-PIPERAZINE-1,4-DICARBOXYLIC ACID 4-BENZYL ESTER 1-TERT-BUTYL ESTER serves as a key intermediate or building block in the synthesis of more complex organic molecules, contributing to the advancement of chemical knowledge and the creation of novel compounds.
Used in Medicinal Chemistry:
(R)-2-METHYL-PIPERAZINE-1,4-DICARBOXYLIC ACID 4-BENZYL ESTER 1-TERT-BUTYL ESTER is utilized as a target molecule in medicinal chemistry, where its structure and properties are investigated to understand its interactions with biological targets and to optimize its pharmacological profile for potential therapeutic applications.
Used in Drug Discovery:
In the process of drug discovery, (R)-2-METHYL-PIPERAZINE-1,4-DICARBOXYLIC ACID 4-BENZYL ESTER 1-TERT-BUTYL ESTER is employed as a candidate molecule, undergoing various screenings and assays to evaluate its efficacy, safety, and pharmacokinetic properties, with the aim of identifying new therapeutic agents.

InChI:InChI=1/C18H26N2O4/c1-14-12-19(10-11-20(14)17(22)24-18(2,3)4)16(21)23-13-15-8-6-5-7-9-15/h5-9,14H,10-13H2,1-4H3/t14-/m1/s1

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 109-07-9 (RS)-2-methylpiperazine 
• 501-53-1 benzyl chloroformate 

Downstream Products

• 1207455-08-0 tert-butyl 4-(4-(9-(4-fluorophenyl)-3-oxo-3,7,8,9-tetrahydro-2H-pyrido[4,3,2-de]phthalazin-8-yl)benzyl)-2-methylpiperazine-1-carboxylate 
• 1207455-06-8 9-(4-fluorophenyl)-8-(4-((3-methylpiperazin-1-yl)methyl)phenyl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one 
• 120737-78-2 tert-butyl 2-methylpiperazine-1-carboxylate 

Relevant academic research and scientific papers

Optimization of 5-substituted thiazolyl ureas and 6-substituted imidazopyridines as potential HIV-1 latency reversing agents

A persistent latent reservoir of virus in CD4+ T cells is a major barrier to cure HIV. Activating viral transcription in latently infected cells using small molecules is one strategy being explored to eliminate latency. We previously described the use of a FlpIn.FM HEK293 cellular assay to identify and then optimize the 2-acylaminothiazole class to exhibit modest activation of HIV gene expression. Here, we implement two strategies to further improve the activation of viral gene expression and physicochemical properties of this class. Firstly, we explored rigidification of the central oxy-carbon linker with a variety of saturated heterocycles, and secondly, investigated bioisosteric replacement of the 2-acylaminothiazole moiety. The optimization process afforded lead compounds (74 and 91) from the 2-piperazinyl thiazolyl urea and the imidazopyridine class. The lead compounds from each class demonstrate potent activation of HIV gene expression in the FlpIn.FM HEK293 cellular assay (both with LTR EC50s of 80 nM) and in the Jurkat Latency 10.6 cell model (LTR EC50 220 and 320 nM respectively), but consequently activate gene expression non-specifically in the FlpIn.FM HEK293 cellular assay (CMV EC50 70 and 270 nM respectively) manifesting in cellular cytotoxicity. The lead compounds have potential for further development as novel latency reversing agents.

Thiazolidine derivatives or salts thereof as an active ingredient an inhibitor Pim

PROBLEM TO BE SOLVED: To provide compounds which have excellent Pim inhibitory action and are useful as pharmaceuticals.SOLUTION: A compound is a thiazolidine derivative represented by the general formula (1) in the figure, or a salt thereof. (In the formula, X represents O or S; Rrepresents a hydrogen atom or a Calkyl group; Z, Z, Z, Z, Zand Zeach independently represent CH or N; Y represents an optionally substituted, divalent Caromatic hydrocarbon group or the like; Am represents a disubstituted amino group, or an optionally substituted, nitrogen-containing saturated heterocyclic group; and Rand Reach independently represent a hydrogen atom, a halogen atom, an alkyl group or the like.)

METHODS OF USING DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY (ADP-RIBOSE)POLYMERASE (PARP)

Provided herein are methods of treating cancer comprising administering a topoisomerase inhibitor, temozolomide, or a platin in combination with a Compound of Formula (I) or Formula (II), where the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein.

DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)

A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.